Preparation of artesunate fat emulsion for injection and application of artesunate fat emulsion in treatment of malaria

A technology of artesunate and water for injection, which is applied in the field of pharmacy, can solve the problems of not being able to be used for injection and not being able to play a role, and achieve the effects of increasing stability, reducing toxic and side effects, and being convenient to use
CN102895186AInactive Publication Date: 2013-01-30福州欣瑞普医药科技有限公司
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Patent Information

Authority / Receiving Office
CN · China
Current Assignee / Owner
福州欣瑞普医药科技有限公司
Publication Date
2013-01-30
Estimated Expiration
Not applicable · inactive patent

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Abstract

The invention discloses an artesunate fat emulsion injection preparation which contains 0.01 to 30 wt% of artesunate, 10.0 to 30.0 wt% of oil for injection, 0.6 to 30.0 wt% of an emulsifier, 0 to 10 wt% of a solubilizer, 0 to 5 wt% of a co-emulsifier, 2.25 to 7 wt% of an isotonic agent and 0.002 to 0.075 wt% of an anti-oxidant, with the balance being injection water. The invention also discloses a preparation method and pharmacodynamic and safety evaluation for the artesunate fat emulsion injection preparation. The artesunate fat emulsion provided by the invention has the characteristics of good biocompatibility, high physical stability, convenient preparation, good security, high drug loading capacity and the like, has a particle size of less than 200 mu m and is suitable for injection, e.g, intravenous injection and intramuscular injection. According to the invention, the characteristic that a soybean oil fat emulsion inhibits growth of plasmodium falciparum is utilized to enhance anti-malarial effects of drugs, to improve bioavailability of the drugs and to reduce toxic and side effects of the drugs; nutrients needed by the body of a patient with malaria can be provided, the activity of lymphocytes of the patient is improved, which assists the patient in resisting malaria and recovering.
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Description

technical field

[0001] The invention belongs to the field of pharmacy, and relates to a fat emulsion injection, in particular to an artesunate fat emulsion injection. Background technique

[0002] Artemisinin is an effective antimalarial monomer isolated and purified from Artemisia annua by Chinese scholars in the early 1970s. It is a new type of sesquiterpene lactone compound containing a peroxide bridge structure. The characteristics of no drug resistance and low toxicity are called "the greatest hope for the treatment of malaria" by the World Health Organization, and can be regarded as the greatest contribution of Chinese pharmaceutical workers to human society. Its discovery has become another important milestone in the world's antimalarial history after quinine. However, studies have shown that taking artemisinin preparations alone for a long time can easily lead to drug resistance of pathogens, and artemisinin is water-soluble and has low bioavailability. Therefore, a...

Claims

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